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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
Published on: November 7, 2025
Cell-based assays in GPCR drug discovery.
1Novartis Institutes for BioMedical Research Basel, Center for Proteomic Chemistry, Novartis Pharma AG, 4002 Basel, Switzerland. sandra.siehler@novartis.com
Biotechnology Journal
|April 3, 2008
Summary
G protein-coupled receptors (GPCRs) are crucial cell surface proteins involved in physiological regulation and targeted by 30% of drugs. This review covers cellular assays for GPCR ligand discovery.
Area of Science:
- Biochemistry
- Pharmacology
- Cell Biology
Background:
- G protein-coupled receptors (GPCRs) are essential cell surface receptors that mediate signal transduction.
- GPCRs feature a characteristic structure with seven transmembrane alpha-helices.
- Their critical roles in physiology and disease make them important drug targets.
Purpose of the Study:
- To review current and emerging cellular assays for GPCR ligand discovery.
- To highlight the significance of GPCRs in drug development.
Main Methods:
- The review synthesizes information on various cellular assay methodologies.
- Focus is placed on assays relevant to identifying ligands for GPCRs.
Main Results:
- GPCRs are implicated in numerous physiological processes and diseases.
- Approximately 30% of currently marketed drugs target GPCRs, underscoring their therapeutic importance.
- A diverse range of cellular assays are available for GPCR research.
Conclusions:
- Cellular assays are vital tools for the discovery of novel GPCR-targeting drugs.
- Continued research into GPCRs and assay development is crucial for advancing therapeutics.
